Pharmaceutical Research

, Volume 30, Issue 1, pp 32–40

Effect of Vehicles on the Maximum Transepidermal Flux of Similar Size Phenolic Compounds

  • Qian Zhang
  • Peng Li
  • David Liu
  • Michael S. Roberts
Research Paper

DOI: 10.1007/s11095-012-0846-x

Cite this article as:
Zhang, Q., Li, P., Liu, D. et al. Pharm Res (2013) 30: 32. doi:10.1007/s11095-012-0846-x

Abstract

Purpose

In principle, maximum transepidermal fluxes of solutes should be similar for different vehicles, except when the solute or vehicle modifies the skin. Here we estimated maximum flux, stratum corneum solubility, diffusivity and permeability coefficient for a range of similarly sized phenolic compounds with varying lipophilicity from polar and lipophilic vehicles.

Methods

Maximum flux and other skin transport parameters through human epidermis were obtained from lipophilic vehicles (mineral oil (MO) and isopropyl myristate (IPM)) and compared with values from water and propylene glycol (PG)-water solutions. Solvent uptake and changes in stratum corneum infrared spectroscopy and multiphoton microscopy imaging were also investigated.

Results

Maximum fluxes for MO and water were similar but IPM has a higher value for more polar phenols due to a higher diffusivity and PG-water had a higher flux due to higher solubility in the stratum corneum. Whereas maximum flux for various phenols was directly related to solubility in the stratum corneum independent of vehicle, increasing phenol lipophilicity increased and decreased permeability coefficient for aqueous solvents and lipophilic solvents, respectively.

Conclusion

The maximum fluxes for phenols with a similar molecular size and varying lipophilicity were comparable between water and MO vehicles but higher for IPM and PG-water mixtures.

KEY WORDS

diffusivity lipophilic vehicle maximum flux permeability coefficient solubility in the stratum corneum 

Abbreviations

ATR-FTIR

attenuated total reflectance Fourier transform infrared

Cv

solute concentration in the vehicle

D*

diffusivity per unit path length

HPLC

high-performance liquid chromatography

IPM

isopropyl myristate

Jmax,estimated

maximum fluxes estimated from dilute solutions

Jss

steady-state flux

KIPM, pool

partition coefficient between IPM lipid pool and usual path for solute diffusion in stratum corneum

kp

permeability coefficient

KSC

stratum corneum-vehicle partition coefficient

log P

logarithmic (base 10) form of octanol-water partition coefficient

MO

mineral oil

PBS

phosphate buffered saline

PG

propylene glycol

Qss

cumulative amount of solute penetrated at steady state

Sv

solute solubility in the vehicle

Sf

solvent factor

SSC

solute solubility in the stratum corneum

tlag

lag time

WF

weight fraction

Copyright information

© Springer Science+Business Media, LLC 2012

Authors and Affiliations

  • Qian Zhang
    • 1
  • Peng Li
    • 1
  • David Liu
    • 2
  • Michael S. Roberts
    • 1
    • 2
  1. 1.School of Pharmacy and Medical SciencesUniversity of South AustraliaAdelaideAustralia
  2. 2.Therapeutics Research Centre, School of Medicine University of QueenslandPrincess Alexandra HospitalWoolloongabbaAustralia

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